Development of small molecular radiolabeled probes for nuclear medical imaging of unstable plaques

2014 Fiscal Year Final Research Report

• Project/Area Number: 24591813
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: National Cardiovascular Center Research Institute (2014); Kyoto University (2012-2013)
• Principal Investigator: TEMMA TAKASHI 独立行政法人国立循環器病研究センター, 研究所, 室長 (90378787)
• Co-Investigator(Kenkyū-buntansha): SAJI Hideo 京都大学, 薬学研究科, 教授 (40115853) ; SHIOMI Masashi 神戸大学, 医学研究科, 准教授 (50226106)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: 放射性医薬品 / 動脈硬化イメージング / 不安定プラーク

Outline of Final Research Achievements

This study aimed to develop small molecular radiolabeled probes for imaging Fatty Acid Binding Protein 4 (FABP4) and Matrix Metalloproteinase 12 (MMP12) in unstable plaques since FABP4 and MMP12 are promising candidates for molecular targeted therapy of atherosclerosis. 125I-TAP1 with triazolopyrimidine structure showed high FABP4 affinity and selectivity but showed high nonspecific accumulation in vitro. 18F-FTAP1 showing lower hydrophobicity rather than 125I-TAP1 maintained high affinity and selectivity toward FABP4 and succeeded in decrease of nonspecific accumulation in vitro. Besides, 18F-FTAP1 enabled in vivo imaging of FABP4 expression in mice by microPET/CT.

Free Research Field

放射性薬品化学・分子イメージング学